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AbstractAimMethodsResultsConclusionTo enhance cefixime’s effectiveness and address drug delivery challenges like concentration at the site, dose, and time, present study investigated the impact of polymer blends on cefixime’s in vitro release profile.Cefixime-loaded nanoparticles were prepared via a modified solvent evaporation method, forming a W/O/W double emulsion. Characterisation included FT-IR, zeta potential, TGA, TEM, and XRD, with in vitro studies and kinetic models used to analyse the release mechanism.The PH-4 nanoparticle formulation (80:20 PCL/HPMC, 0.5% PVA) achieved an 81% loading rate, no adverse effects, and a controlled release of 84.66%±2.53 over 30 days. It showed stable physicochemical properties, with in vitro antibacterial tests revealing inhibition zones of 27.4 ± 2.12 mm for E. coli and 17.2 ± 2.23 mm for S. aureus at 12 hours.Based on the findings, developed nanoparticulate system containing PCL/HPMC demonstrates its efficacy and safety as a controlled drug delivery method for antibiotics like cefixime. [ABSTRACT FROM AUTHOR]

Despite the availability of a number of efficacious treatments for Parkinson's disease, their limitations and drawbacks, particularly related to low brain bioavailability and associated side effects, emphasize the need for alternative and more effective therapeutic approaches. Nanomedicine, the application of nanotechnology in medicine, has received considerable interest in recent years as a method of effectively delivering potentially therapeutic molecules to the brain. In particular, polymeric nanoparticles, constructed from biodegradable polymer, have shown great promise in enhancing therapeutic efficacy, reducing toxicity, and ensuring targeted delivery. However, their clinical translation remains a considerable challenge. This article reviews recent in vitro and in vivo studies using polymeric nanoparticles as drug and gene delivery systems for Parkinson's disease with their challenges and future directions. We are also particularly interested in the technical properties, mechanism, drugs release patterns, and delivery strategies to overcome the blood–brain barrier. © 2024 International Parkinson and Movement Disorder Society. [ABSTRACT FROM AUTHOR]

The treatment of brain tumors has been predominantly hindered by the limited ability of drugs to penetrate the blood-brain barrier. However, recent advancements in nanotechnology have presented a therapeutic potential by facilitating the delivery of drugs and macromolecules across the blood-brain barrier. These nanotechnology-enabled treatments target tumor cells, exploit tumor biology, enhance the pharmacokinetic properties of drugs, and minimize off-target side effects. Nanotechnology provides efficacy and safety of nano-enabled therapies for treating brain tumors. HIGHLIGHTS: Nanotechnology-enabled therapies offer potential for blood-brain barrier challenges. Nanotechnology-enabled therapies facilitate drug and macromolecule delivery to the brain. Nanotechnology enables targeted delivery to tumor cells, leveraging tumor biology. Nanotechnology improves pharmacokinetics and reduces off-target side-effects. Nanotechnology offers efficacy and safety of nano-enabled therapies for brain tumors. [ABSTRACT FROM AUTHOR]

Lipid nanoparticles (LNPs) are the most clinically advanced RNA delivery technology, but their efficiency is limited by low RNA release after endosome disruption. To improve RNA release, an acid‐responsive polymer is synthesized with which to formulate LNPs for RNA encapsulation and release. Specifically, three acid‐responsive poly(lactic acid)‐block‐poly(carboxybetaine) zwitterionic derivatives are designed and synthesized that are cationic and complexed with RNA at pH 7.4, but are neutral following cleavage at endosomal pH, thereby having lower affinity to RNA. The polymers are formulated into each of the clinically approved Onpattro, Moderna, or Pfizer LNP formulations to produce hybrid polymer‐lipid nanoparticles (PLNPs). With the PLNPs, the IC50 values of multiple small interfering RNAs (siRNAs) decreased up to 5.4‐fold compared to parent LNPs in several cell lines. Moreover, messenger RNA (mRNA) transfection increased up to two fold. The acid‐responsive polymers in PLNPs accounted for the enhanced RNA transfection as this phenomenon is lost with acid‐inert polymers. Confocal microscopy confirmed that cytosolic RNA concentration increased using the acid‐responsive polymers; conversely, uptake and endosomal escape are identical to existing LNPs. This confirmed that enhanced RNA transfection is due to increased RNA dissociation from its carrier. The novel polymer represents a versatile strategy to increase RNA transfection from LNPs. [ABSTRACT FROM AUTHOR]

Polymer gels are fascinating soft materials and have become excellent candidates for wearable electronics, biomedicine, sensors, etc. Synthetic gels usually suffer from poor mechanical properties, and integrating good mechanical properties, adhesiveness, stability, and self‐healing performances in one gel is more difficult. Herein, polymerization‐induced self‐assembly (PISA) providing PEG‐gels with an overall improvement in their comprehensive performances is reported. PISA synthesis is carried out in PEG (solvent) to efficiently produce various nanoparticles, which are used as the nanofillers in the subsequent synthesis of PEG‐gels with dynamic micelle‐crosslinked hierarchical structures. Compared to hydrogels, PEG‐gels show excellent long‐term stability due to the nonvolatile feature of PEG solvent. The hierarchical PEG‐gels (with nanofillers) exhibit better mechanical and adhesive properties than the homogeneous‐gels (without nanofillers). The energy dissipation mechanism of the PEG‐gels is analyzed via stress relaxation and cyclic mechanical tests. High‐density hydrogen bonds between the micelles and PAA matrix can be broken and reformed, endowing better self‐healing properties of the dynamic micelle‐crosslinked PEG gels. This work provides a simple strategy for producing hierarchical structural gels with enhanced properties, which offers fundamentals and inspirations for the designing of various advanced functional materials. [ABSTRACT FROM AUTHOR]

Covalent drugs can offer significant advantages over non-covalent drugs in terms of pharmacodynamics (i.e., target-binding properties). However, the development of covalent drugs is sometimes hampered by pharmacokinetic limitations (e.g., low bioavailability, rapid metabolism and toxicity due to off-target binding). Polymeric nanoparticles offer a potential solution to these limitations. Delivering covalent drugs via polymeric nanoparticles provides myriad benefits in terms of drug solubility, permeability, lifetime, selectivity, controlled release and the opportunity for synergistic administration alongside other drugs. In this short review, we examine each of these benefits in turn, illustrated through multiple case studies. [ABSTRACT FROM AUTHOR]

Objective(s): Using a quality-by-design methodology, the current research is aimed to prepare and enhance the PEGylated PLGA-loaded regorafenib monohydrate polymeric nanoparticles for enhancing oral bioavailability and biopharmaceutical attributes. The oral multi-kinase inhibitor inhibits VEGFR2-TIE2 tyrosine kinases on two separate targets, which results in anti-angiogenic activity. It also inhibits stromal and oncogenic receptor tyrosine kinases. Materials and Methods: The current study developed nanosized, biocompatible, and PEGylated PLGA polymeric nanoparticles to administer regorafenib monohydrate to patients with metastatic colon cancer. This was accomplished using a modified nanoprecipitation technique to make drug-encapsulated PEGylated PLGA nanoparticles with poloxamer 188 as a stabilizer. Results: The polymeric nanoformulations were characterized for zeta potential, distribution of particle size, entrapment efficiency, DSC, FT-IR, X-RD, and SEM. Both in vitro and in vivo experimental studies were performed for the pure drug and the improved nanoparticle formulation. Conclusion: The nanoparticles obtained from optimization studies were found to have smaller particle sizes, higher entrapment efficiency (%), drug loading capacity, spherical shape particles, amorphous drug embedded matrix, and a biphasic delayed release pattern. These findings suggest that drug-loaded PEGylated PLGA nanoparticles are a potent formulation for the treatment of colon cancer, with improved oral bioavailability and biopharmaceutical properties. [ABSTRACT FROM AUTHOR]

Background/Objectives: Conventional anticancer therapies often lack specificity, targeting both cancerous and normal cells, which reduces efficacy and leads to undesired off-target effects. An additional challenge is the presence of hypoxic regions in tumors, where the Hypoxia Inducible Factor (HIF) transcriptional system drives the expression of pro-survival and drug resistance genes, leading to radio- and chemo-resistance. This study aims to explore the efficacy of targeted nanoparticle (NP)-based small interfering RNA (siRNA) therapies in downregulating these genes to enhance treatment outcomes in pancreatic cancer, a tumor type characterized by high CD44 expression and hypoxia. Methods: We utilized hyaluronic acid (HA)-displaying nanoparticles composed of positively charged chitosan (CS) complexed with siRNA to target and knock down HIF-1α in pancreatic cancer cells. Two NP formulations were prepared using either low molecular weight (LMW) or high molecular weight (HMW) CS. These formulations were evaluated for their internalization by cells and their effectiveness in gene silencing, both in vitro and in vivo. Results: The study found that the molecular weight (MW) of CS influenced the interaction between HA and CD44, as well as the release of siRNA upon internalization. The LMW CS formulation shows faster uptake kinetics, while HMW CS is more effective in gene knockdown across different cell lines in vitro. In vivo, both were able to significantly knockdown HIF-1α and some of its downstream genes. Conclusions: The results suggest that HMW and LMW CS-based NPs exhibit distinct characteristics, showing that both MWs have potential for targeted pancreatic cancer therapy by influencing different aspects of delivery and gene silencing, particularly in the hypoxic tumor microenvironment. [ABSTRACT FROM AUTHOR]

Background/Objectives: Cancer remains one of the leading causes of death, with breast, liver, and pancreatic cancers significantly contributing to this burden. Traditional treatments face issues including dose-limiting toxicity, drug resistance, and limited efficacy. Combining therapeutic agents can enhance effectiveness and reduce toxicity, but separate administration often leads to inefficiencies due to differing pharmacokinetics and biodistribution. Co-formulating hydrophobic chemotherapeutics such as paclitaxel (PTX) and hydrophilic immunologic agents such as polyinosinic-polycytidylic acid (Poly IC) is particularly challenging due to their distinct physicochemical properties. This study presents a novel and efficient approach for the co-delivery of PTX and Poly IC using chitosan-based nanoparticles. Method: Chitosan-PEG (CP) nanoparticles were developed to encapsulate both PTX and Poly IC, overcoming their differing physicochemical properties and enhancing therapeutic efficacy. Results: With an average size of ~100 nm, these nanoparticles facilitate efficient cellular uptake and stability. In vitro results showed that CP-PTX-Poly IC nanoparticles significantly reduced cancer cell viability in breast (4T1), liver (HepG2), and pancreatic (Pan02) cancer types, while also enhancing dendritic cell (DC) maturation. Conclusions: This dual-modal delivery system effectively combines chemotherapy and immunotherapy, offering a promising solution for more effective cancer treatment and improved outcomes. [ABSTRACT FROM AUTHOR]

Niosomal and Polymeric-based nanoparticles offer advantages over conventional systems, such as targeted drug delivery and reduced toxicity. These nanoparticles are very promising due to their high drug loading capacity, stability, and ability to target specific cells or tissues. However, developing these nanoparticles presents challenges and requires careful selection of materials. These particles can deliver both hydrophilic and hydrophobic drugs and have applications in cancer therapy, gene therapy, and vaccination. This review aims to provide a comprehensive understanding of the current state of the art in the field of niosomal and polymeric nanoparticle design and optimization for efficient targeted drug delivery. [ABSTRACT FROM AUTHOR]

Vulvovaginal candidiasis (VVC) alters the innate cervicovaginal immunity, which provides an important barrier against viruses and other infections. The incidence of this disease has not decreased in the last 30 years, so effective treatments are still needed. Nanoparticles (NPs) of cellulose acetate phthalate (CAP) and clotrimazole (CLZ) were prepared by the emulsification-diffusion method. NPs were characterized using dynamic light scattering, atomic force microscopy and differential scanning calorimetry; their release profile was determined by the dialysis bag technique and mucoadhesion was evaluated with the mucin-particle method. The growth inhibition study of Candida albicans was carried out using the plate counting technique. Finally, accelerated physical stability tests of NPs were carried out, both in water and in SVF. The CAP-CLZ NPs had an average diameter of 273.4 nm, a PDI of 0.284, smooth surfaces and spherical shapes. In vitro release of CLZ from the CAP NPs was categorized with the Weibull model as a matrix system in which initial release was rapid and subsequently sustained. The inhibition of C. albicans growth by the CAP-CLZ NPs was greater than that of free CLZ, and the CAP-only NPs had a microbicidal effect on C. albicans. The NPs showed poor mucoadhesiveness, which could lead to studies of their mucopenetration capacities. An accelerated physical stability test revealed the erosion of CAP in aqueous media. A nanoparticulate system was developed and provided sustained release of CLZ, and it combined an antifungal agent with a microbial polymer that exhibited antifungal activity against C. albicans. [ABSTRACT FROM AUTHOR]

Chemotherapy is one of the most common therapeutic approaches in most cancers like prostate cancer, which has always faced limitations. The purpose of the present study was to design and prepare the targeted polymeric nanoparticles for the co-delivery of Paclitaxel (PTX) and Chrysin (CHR) to prostate cancer cells to improve the PTX therapeutic efficacy. Through the current research, the surface modification of the PTX/CHR-loaded PCL-PEG-PCL nanoparticles with chitosan and hyaluronic acid (PTX/CHR-PCEC-CS/HA) was successfully performed through the physical adsorption process. SEM results showed that this polymeric NPs had a homogeneous spherical structure. The encapsulation efficiency was 78.6 and 93.28% for CHR and PTX, respectively. It is important to mention that the controlled drug-release behavior of the PTX/CHR-PCEC-CS/HA was also investigated. The results demonstrated that the dual drug-loaded PCEC-CS/HA NPs had a significant effect on reducing the survival of the cancer. Also, the results exhibited that the cytotoxicity of the dual drug-loaded polymeric NPs in the PC3 cell line is significantly higher than in the HUVEC cell line. Based on the findings, the targeted PTX/CHR-PCEC-CS/HA NPs could be employed as a suitable candidate for the effective treatment of the prostate cancer. [ABSTRACT FROM AUTHOR]

Cancer nanomedicines, characterized by submicrometer-sized formulations, aim to optimize the biodistribution of anticancer drugs by minimizing off-target effects, reducing toxicity, enhancing target site accumulation, and improving overall efficacy. Numerous nanomedicines have been developed to improve the effectiveness and safety of traditional anticancer treatments. These include formulations with carbon nanotubes, nanodiamonds, enzyme-responsive nanoparticles for controlled drug release, dendrimers as nanoparticle drug carriers, quantum dot nanocarrier systems for precise drug delivery, solid lipid nanoparticles, and polymeric nanoparticles designed for targeted drug delivery. Additionally, nanotechnology has been explored in cancer treatment through gene therapy. Despite these advances, the complex nature of carrier materials and functional integration presents challenges in preparing these candidates for clinical translation. Nanotechnology, with its unique features at the nanoscale, offers novel possibilities for developing cancer therapies while increasing efficacy and safety. Although only a few nanotherapeutics have obtained clinical approval, exciting uses for nanotechnology are on the horizon. Nanoparticles possess unique transport, biological, optical, magnetic, electrical, and thermal capabilities due to their small size within the light wavelength spectrum. This results in high surface area-to-volume ratios, allowing for the incorporation of various supporting components in addition to active medicinal substances. These properties aid in solubilization, degradation protection, delayed release, immune response evasion, tissue penetration, imaging, targeted distribution, and triggered activation. In summary, the future of nanomedicine holds promise for introducing innovative platforms in cancer treatment. The research presented underscores the potential for nanoparticles to revolutionize anticancer therapies, enhancing the overall therapeutic approach. [ABSTRACT FROM AUTHOR]

This paper may be the first meta-analysis that presents a comprehensive synthesis of scientific works spanning the last five years, focusing on methodologies and results related to the analysis of nanocomposite using nanoparticles. The primary objective is to identify the optimal algorithm using software information and leading to better classification methodology. Specifically, this study comes up with the advantages and the drawbacks of the most used algorithms and proposes an enhancement and performance of Recurrent Neural Networks based on Long Short Term Memory (LSTM) neurons. Besides, a comparison of Deep Learning methods for the classification of polymeric nanoparticles, with polypropylene serving as a case study will be implemented. Experiment comparisons are conducted to assess with one physical property, later expanded to four properties and finally to eight properties. Neural networks, including Artificial Neural Networks (ANN), Recurrent Neural Networks (RNN), and Recurrent Neural Networks-Monte Carlo, are employed for simulations. The evaluation criteria encompass accuracy, calculation time, mean square error (MSE) and other metrics. The findings contribute to the selection of an optimal algorithm for the analysis of polymeric nanoparticles, emphasizing the potential of Deep Learning methodologies, particularly Recurrent Neural Networks Monte Carlo, in advancing classification accuracy and efficiency.

Dynamic Covalent Chemistry (DCC) enables the development of responsive molecular systems through the integration of reversible bonds at the molecular level. These systems are thermodynamically stable and capable of undergoing various molecular assemblies and transformations, allowing them to adapt to changes in environmental conditions like temperature and pH. Introducing DCC into the field of polymer science has led to the design of Single-Chain Nanoparticles (SCNPs), which are formed by self-folding via intramolecular crosslinking mechanisms. Defined by their adaptability, SCNPs mimic biopolymers in size and functionality. Biodynamers, a subclass of SCNPs, are specifically designed for their stimuli-responsive and tunable, dynamic properties. Mimicking complex biological structures, their scope of application includes target-specific and pH-responsive drug delivery, enhanced cellular uptake and endosomal escape. In this manuscript, we discuss the integration of DCC for the design of SCNPs, focusing particularly on the characteristics of biodynamers and their biomedical and pharmaceutical applications. By underlining their potential, we highlight the factors driving the growing interest in SCNPs, providing an overview of recent developments and future perspectives in this research field. [ABSTRACT FROM AUTHOR]

Immunotherapy has emerged as a promising approach to cancer treatment, offering improved survival rates and enhanced patients' quality of life. However, realizing the full potential of immunotherapy in clinical practice remains a challenge, as there is still plenty of room for modulating the complexity of the human immune system in favor of an antitumor immunogenicity. Nanotechnology, with its unique properties, holds promise in augmenting the efficacy of cancer immunotherapies in biotherapeutic protection and site- and time-controlled delivery of the immune modulator biologicals. Polymeric nanoparticles are promising biomaterials among different nanocarriers thanks to their robustness, versatility, and cost-efficient design and production. This perspective paper overviews critical concepts in nanometric advanced delivery systems applied to cancer immunotherapy. We focus on a detailed exploration of the current state of the art and trends in using poly(beta-aminoester) (pBAE) polymers for nucleic acid-based antitumor immunotherapies. Through different examples of the use of pBAE polymers reported in the literature, we revise the main advantages these polymers offer and some challenges to overcome. Finally, the paper provides insights and predictions on the path toward the clinical implementation of cancer nano-immunotherapies, highlighting the potential of pBAE polymers for advancements in this field. [ABSTRACT FROM AUTHOR]

Abstract Background Hepatic cancer endures a major health scourge as the consequence of a high incidence of > 1 million cases by 2025. Plant-based products are typically effective in ameliorating health conditions. Pomegranate peel extract (PE) with its high polyphenolic content has anticancer effects against different types of cancer. Herein, we aimed to maximize the PE chemotherapeutic efficacy by loading it in a suitable delivery system to overcome the limitations of PE, to control its release and to achieve liver targeting. Method A nanoprecipitation procedure was adopted to incorporate PE into biodegradable and biocompatible natural polymeric zein (ZN)-based nanoparticles (NPs) (PE-ZN NPs). A full factorial design (22 × 31) was developed to study the effects of the formulation variables, namely pH of dispersion, PE-to-ZN ratio and surfactant concentration. Results The optimization revealed a surfactant-free stable PE-ZN NPs formula with a small particle size of 99.5 ± 6.43 nm, high PE encapsulation efficiency % of 99.31% ± 3.64 (w/w) and controlled release of PE over 24 h. Conclusion Moreover, the cytotoxicity of the optimum formula against hepatic cancer HepG2 cell lines was assessed and attained about a 2.5-fold reduction in the inhibitory concentration (IC50) values compared to the free PE affording a promising green platform to combat hepatic cancer. Graphical abstract

Amphiphilic molecules can self-assemble into a wide range of morphologies, making them a promising candidate for drug delivery. Poly-(lactic-co-glycolic acid)–poly-(ethylene glycol) methyl ether (PLGA-MPEG), which is an amphiphilic copolymer, is a broadly used biodegradable drug carrier for drug delivery systems. In this study, computational molecular dynamics (MD) simulations were used to tailor polymeric nanoparticles with improved drug delivery efficacy. To optimize drug loading, customized copolymers with varying lactic acid to glycolic acid ratios, as well as the length of the MPEG chain, were considered. These simulations were carried out with varying amounts of the drug and copolymers. Our findings suggest the optimized conditions under which gemcitabine (GEM) was efficiently encapsulated in polymeric nanoparticles. The simulations reveal that varying the proportions of lactic and glycolic acid and MPEG chain lengths in copolymers can improve drug encapsulation efficiency. Increasing the glycolic content of the copolymers resulted in better GEM encapsulation, which corresponded to a higher binding energy. The strong interaction energy between GEM and the glycolic acid-rich copolymer suggested that the drug might have a slow-release profile. GEM and PLGGA-MPEGn have a higher average number of hydrogen bonds than that with PLGA-MPEGn and PLLGA-MPEGn. This indicates that the copolymer's flexibility increased as the concentration of glycolic acid in the copolymer increased, promoting the better formation of polymeric nanoparticles. This study has the potential to pave the way for the fabrication of polymeric nanocarriers capable of efficiently encapsulating drugs. [ABSTRACT FROM AUTHOR]

The World Health Organization (WHO) reported that of all the non-communicable diseases, cancer is considered the second cause of death worldwide. This has driven the big pharma companies to prioritise anticancer products in their pipeline. In addition, research has focused on exploration of new anticancer molecules and design of suitable dosage forms to achieve effective drug delivery to the tumour site. Nanotechnology is a valuable tool to build nano delivery systems with controlled and targeted drug release properties. Nanoparticles can be fabricated by robust, scalable and economic techniques using various polymers. Moreover, specific functional groups can be introduced to the surface of nanoparticles enabling targeting to a specific tissue; besides, they exhibit versatile drug release patterns according to the rate of polymer degradation. This review outlines the processes and advances in surface functionalisation of nanoparticles employed for treatment of breast cancer. The therapeutic molecules, the polymers used to fabricate nanoparticles, the techniques used to prepare the nanoparticles have been reviewed with a focus on the processes employed to functionalise these nanoparticles with suitable ligands to target different types of breast cancer. [ABSTRACT FROM AUTHOR]

This paper presents an experimental study on preparation of tramadol hydrochloride (TrH) loaded nanoparticles, and stability determination in various infusion solutions. In this study, various nanoparticle preparation parameters based on w/o/w emulsification solvent evaporation method, including stabilizer type, stabilizer concentration, polymer concentration, homogenization speed and initial drug amount were systematically tested to verify their versatility for preparing nanoparticles. Initially both particle size and encapsulation efficiency of nanoparticles were changed significantly with the change in surfactant and polymer ratio (p<0.05). However, homogenization speed only changed particle size (average size 339.3±1.8 nm for 15000 rpm, 318.9±6.4 nm for 20000 rpm and 237.2±7.8 nm for 25000 rpm) (p<0.05) and initial drug concentration is only affected the encapsulation efficiency (34.2±0.7% for 4 mg/mL and 33.2±0.9 for 1.6 mg/mL) (p<0.05). Storage at room temperature for 3 months resulted in an increase in particle size and polydispersity index. Prepared nanoparticles showed the best stability after storage at – 20 °C for in 3 months. Finally, storage of nanoparticles in various infusion solutions resulted an undesirable changes for 6% Hydroxyethyl starch in 0.9% sodium chloride injection, 10% Dextran 40 and 4% Succinyl gelatin solutions. It was shown that an appropriate delivery of TrH loaded PLGA nanoparticles as infusion can be prepared only in water for injection, 20% Mannitol, 0.9% Sodium chloride and 5% Dextrose solutions. [ABSTRACT FROM AUTHOR]

The pH- and thermo-responsive behavior of polymeric hydrogels M C − c o − M A have been studied in detail using dynamic light scattering D L S , scanning electron microscopy   S E M , nuclear magnetic resonance (1H NMR) and rheology to evaluate the conformational changes, swelling–shrinkage, stability, the ability to flow and the diffusion process of nanoparticles at several temperatures. Furthermore, polymeric systems functionalized with acrylic acid M C and acrylamide M A were subjected to a titration process with a calcium chloride C a C l 2 solution to analyze its effect on the average particle diameter   D z , polymer structure and the intra- and intermolecular interactions in order to provide a responsive polymer network that can be used as a possible nanocarrier for drug delivery with several benefits. The results confirmed that the structural changes in the sensitive hydrogels are highly dependent on the corresponding critical solution temperature C S T of the carboxylic (–COOH) and amide (–CONH2) functional groups and the influence of calcium ions C a 2 + on the formation or breaking of hydrogen bonds, as well as the decrease in electrostatic repulsions generated between the polymer chains contributing to a particle agglomeration phenomenon. The temperature leads to a re-arrangement of the polymer chains, affecting the viscoelastic properties of the hydrogels. In addition, the diffusion coefficients D of nanoparticles were evaluated, showing a closeness among with the morphology, shape, size and temperature, resulting in slower diffusions for larger particles size and, conversely, the diffusion in the medium increasing as the polymer size is reduced. Therefore, the hydrogels exhibited a remarkable response to pH and temperature variations in the environment. During this research, the functionality and behavior of the polymeric nanoparticles were observed under different analysis conditions, which revealed notable structural changes and further demonstrated the nanoparticles promising high potential for drug delivery applications. Hence, these results have sparked significant interest in various scientific, industrial and technological fields. [ABSTRACT FROM AUTHOR]

In this work, we developed multifunctional hydrogel nanoparticles (NPs) that can encapsulate anticancer drugs and imaging contrast agents as well. Mitomycin C (MMC) and rhodamine B (RB) were selected as models for anticancer drugs and imaging contrasting agents, respectively. Both MMC and RB were linked to the succinated polyvinyl alcohol polymer (PVA-SA). The selected labeled hydrogel NPs ((0.5% RB)-PVA-SA NPs and (1.5% RB)-PVA-SA NPs) improved the RB quantum yield from 29.8% to a minimum of 42.7%. Moreover, they showed higher emission stability compared to free RB when they were repeatedly excited at 554 nm for 2 h. Furthermore, the dye polymeric interactions significantly increased the RB fluorescence lifetime by approximately twofold. All these optical properties pave the way for our labeled hydrogel NPs to be used in imaging-guided therapy. For the labeled MMC-loaded NPs, the MMC-binding efficiency was found to be exceedingly high in all synthesized samples: a minimum of 92% was achieved. In addition, the obtained pH-dependent drug release profiles as well as the cytotoxicity evaluation demonstrated the high potential of releasing MMC under acidic cancerous conditions. Moreover, the in vitro cellular uptake experiment confirmed the accumulation of MMC NPs throughout the cytoplasm. [ABSTRACT FROM AUTHOR]

The aggregation-caused quenching (ACQ) rationale has been employed to improve the fluorescence imaging accuracy of nanocarriers by precluding free probe-derived interferences. However, its usefulness is undermined by limited penetration and low spatiotemporal resolution of NIR-I (700–900 nm) bioimaging owing to absorption and diffraction by biological tissues and tissue-derived autofluorescence. This study aimed to develop ACQ-based NIR-II (1000–1700 nm) probes to further improve the imaging resolution and accuracy. The strategy employed is to install highly planar and electron-rich julolidine into the 3,5-position of aza-BODIPY based on the larger substituent effects. The newly developed probes displayed remarkable photophysical properties, with intense absorption centered at approximately 850 nm and bright emission in the 950–1300 nm region. Compared with the NIR-I counterpart P2, the NIR-II probes demonstrated superior water sensitivity and quenching stability. ACQ1 and ACQ6 exhibited more promising ACQ effects with absolute fluorescence quenching at water fractions above 40% and higher quenching stability with less than 2.0% fluorescence reillumination in plasma after 24 h of incubation. Theoretical calculations verified that molecular planarity is more important than hydrophobicity for ACQ properties. Additionally, in vivo and ex vivo reillumination studies revealed less than 2.5% signal interference from prequenched ACQ1, in contrast to 15% for P2. Novel aggregation-caused quenching (ACQ) probes with bright NIR-II fluorescence were developed by incorporating highly planar and electron-rich julolidine at the 3,5-position of aza-BODIPY, improving the fluorescence imaging accuracy of nanocarriers. [Display omitted] [ABSTRACT FROM AUTHOR]

Background: Hepatic cancer endures a major health scourge as the consequence of a high incidence of > 1 million cases by 2025. Plant-based products are typically effective in ameliorating health conditions. Pomegranate peel extract (PE) with its high polyphenolic content has anticancer effects against different types of cancer. Herein, we aimed to maximize the PE chemotherapeutic efficacy by loading it in a suitable delivery system to overcome the limitations of PE, to control its release and to achieve liver targeting. Method: A nanoprecipitation procedure was adopted to incorporate PE into biodegradable and biocompatible natural polymeric zein (ZN)-based nanoparticles (NPs) (PE-ZN NPs). A full factorial design (22 × 31) was developed to study the effects of the formulation variables, namely pH of dispersion, PE-to-ZN ratio and surfactant concentration. Results: The optimization revealed a surfactant-free stable PE-ZN NPs formula with a small particle size of 99.5 ± 6.43 nm, high PE encapsulation efficiency % of 99.31% ± 3.64 (w/w) and controlled release of PE over 24 h. Conclusion: Moreover, the cytotoxicity of the optimum formula against hepatic cancer HepG2 cell lines was assessed and attained about a 2.5-fold reduction in the inhibitory concentration (IC50) values compared to the free PE affording a promising green platform to combat hepatic cancer. [ABSTRACT FROM AUTHOR]

Chagas disease (CD) is a worldwide public health problem. Benznidazole (BZ) is the drug used to treat it. However, in its commercial formulation, it has significant side effects and is less effective in the chronic phase of the infection. The development of particulate systems containing BZ is therefore being promoted. The objective of this investigation was to develop polymeric nanoparticles loaded with BZ and examine their trypanocidal impact in vitro. Two formulas (BNP1 and BNP2) were produced through double emulsification and freeze drying. Subsequent to physicochemical and morphological assessment, both formulations exhibited adequate yield, average particle diameter, and zeta potential for oral administration. Cell viability was assessed in H9C2 and RAW 264.7 cells in vitro, revealing no cytotoxicity in cardiomyocytes or detrimental effects in macrophages at specific concentrations. BNP1 and BNP2 enhanced the effect of BZ within 48 h using a treatment of 3.90 μg/mL. The formulations notably improved NO reduction, particularly BNP2. The findings imply that the compositions are suitable for preclinical research, underscoring their potential as substitutes for treating CD. This study aids the quest for new BZ formulations, which are essential in light of the disregard for the treatment of CD and the unfavorable effects associated with its commercial product. [ABSTRACT FROM AUTHOR]

Cancer immunotherapy has revolutionized oncology by harnessing the patient's immune system to target and eliminate cancer cells. However, immune checkpoint blockades (ICBs) face limitations such as low response rates, particularly in immunologically 'cold' tumors. Enhancing tumor immunogenicity through immunogenic cell death (ICD) inducers and advanced drug delivery systems represents a promising solution. This review discusses the development and application of various nanocarriers, including polymeric nanoparticles, liposomes, peptide-based nanoparticles, and inorganic nanoparticles, designed to deliver ICD inducers and ICBs effectively. These nanocarriers improve therapeutic outcomes by converting cold tumors into hot tumors, thus enhancing immune responses and reducing systemic toxicity. By focusing on single-nanoparticle systems that co-deliver both ICD inducers and ICBs, this review highlights their potential in achieving higher drug concentrations at tumor sites, improving pharmacokinetics and pharmacodynamics, and facilitating clinical translation. Future research should aim to optimize these nanocarrier systems for better in vivo performance and clinical applications, ultimately advancing cancer immunotherapy. [ABSTRACT FROM AUTHOR]

Polymeric nanotheranostics have emerged as promising vehicles for diagnosis‐cum‐targeted therapy in solid tumors, offering precise delivery of therapeutic agents at the site of solid tumors and minimizing systemic side effects. This article summarizes the latest developments in using polymeric nanoparticles for specific treatment strategies in solid tumors. It explores the various methods these nanoparticles utilize for targeted medication delivery. This includes passive targeting through the amplified permeability and retention effect, active targeting via interactions between ligands and receptors, and stimuli‐responsive release mechanisms such as pH, temperature, and enzymatic triggers. Furthermore, we highlight recent developments in stimuli‐responsive polymeric nanoparticles, which enable controlled drug release in response to specific cues in the tumor microenvironment, thus enhancing therapeutic efficacy. Also, we focus on the theranostic polymeric nanoparticles, which are used for diagnosing and treating solid tumors. We discuss critical regulatory considerations and the regulatory bodies of different countries that regulate nanomedicines' safety, efficacy, quality, and manufacturing processes. Overall, this review provides insights into the latest innovations in polymeric nanoparticles for targeted therapy in solid tumors, elucidating their mechanisms of action, stimuli‐responsive properties, and regulatory pathways, which collectively contribute to developing effective and safe nanomedicines for cancer treatment. [ABSTRACT FROM AUTHOR]

The remarkable ability of the human immunodeficiency virus (HIV) to evade the host's immune system and conventional antiretroviral therapy, has posed significant challenges in achieving complete eradication of the virus in people living with HIV (PLWHIV). However, nanotechnology has emerged as promising avenue for addressing some of the obstacles associated with the use of antiretroviral drugs by modifying drug molecules in nanoscale dimensions. Hence, the present study explores the utilization of poly(epsilon‐caprolactone) (PCL) as a carrier for encapsulating tenofovir disoproxil fumarate (TDF), offering an alternative treatment approach for HIV infection. TDF‐loaded polymeric nanoparticles were successfully prepared using double emulsion solvent evaporation technique and characterized. The characterization of TDF‐loaded polymeric nanoparticles at varied drug to polymer ratios showed that TDF was loaded in PCL with an encapsulation efficiency and drug loading capacity in the range of 23–46% and 4.8–19.9%, respectively. Of note, the neutralization efficacy of TDF‐loaded polymeric nanoparticles was more improved compared to free TDF. Encapsulation of TDF with PCL did not hinder the antiviral activity of TDF against HIV‐1 infection but rather enhanced its potency. [ABSTRACT FROM AUTHOR]

The utilization of advanced polymeric materials has indeed emerged as a significant trend in sustainable agriculture, offering a range of innovative applications aimed at enhancing productivity, minimizing environmental impact, and promoting resource efficiency. Smart polymeric materials enable the controlled release of pesticides, herbicides, and fertilizers, thereby enhancing their efficacy while reducing the quantities needed. Superabsorbent polymeric materials act as soil conditioners, assisting in alleviating the negative impacts of drought by retaining moisture and enhancing soil structure. This fosters improved plant growth and resilience in water-scarce environments. Polycationic polymers play a role in plant bioengineering, facilitating genetic transformation processes aimed at enhancing crop productivity and disease resistance. Advanced polymeric systems contribute to the arsenal of precision agriculture tools by enabling precise delivery and targeted application of agricultural inputs. This approach enhances resource efficiency, reduces waste, and minimizes environmental impact while optimizing crop yields. In reviewing recent developments in the design and application of advanced polymeric systems for precision agriculture, several key considerations emerge.

AbstractBreast cancer is one of the most devastating cancers that have no cure. Many therapeutic and diagnostic strategies have been extensively studied in the past decade. Cancer nanotechnology has developed as a promising approach in preclinical examinations, allowing for the early exposure of primary tumors and metastases and the efficient destruction of cancer cells. The current study aims to fabricate and analyze polymeric nanoparticles for breast cancer therapy established on a copolymeric block of α-tocopheryl polyethylene glycol 1000-b-polycaprolactone (TPGS-b-PCL) incorporating paclitaxel (PTX) (termed as T-b-P@PTX). Characterization of the physical, chemical, and structural properties and the in vitro biological activity of TPGS-b-PCL (T-b-P@PTX) obtained by the nanoprecipitation method. The in vitro cytotoxicity of the nanoparticles was explored by MTT assay using MCF-7 breast cancer cells in a time-dependent manner. The IC50 values T-b-P@PTX for MCF-7 cells 543.7 ± 2.58, 130.2 ± 3.54, 66.99 ± 3.43 in 24, 48, 72-h. Biochemical experiments showed that T-b-P@PTX has a strong ability to induce cell death and to be internalized in the MCF-7 cells. Ethidium bromide (EB)-acridine orange (AO) and nuclear DAPI staining methods investigated the morphological changes of the cells. Considering all the advantages, Paclitaxel-loaded T-b-P@PTX polymeric nanoparticle is a promising approach for treating breast cancer.

Abstract(–)-Epigallocatechin-3-gallate (EGCG), a bioactive polyphenol of green tea, has chemo-preventive effects against various cancer cells. Nanoparticles (NPs) carrying different ligands are able to specifically interact with their receptors on different cancer cells that can provide effective release of cytotoxic drugs. In the present study, we have prepared EGCG entrapped NPs using PLGA (poly(d,l-lactide-co-glycolide)). Polyethylene glycol (PEG) and folic acid (FA) via double emulsion solvent evaporation (DESE) method obtained PLGA-EGCG (P-E), PLGA-PEG-EGCG (PP-E), and PLGA-PEG-FA-EGCG (PPF-E). Nanoformulations had been characterized with 1H NMR and FT-IR techniques, AFM, and DLS. PPF-E NPs showed an average size of 220 nm. Analysis of zeta potential confirmed the stability of NPs. HCT-116, HT-29, HCT-15, and HEK 293 cells were treated with both the prepared NPs and free EGCG (0–140 μM). Result showed PPF-E NPs had improved delivery, uptake and cell cytotoxicity toward human folic acid receptor-positive (FR+) colorectal cancer (CRC) cells as mainly on HCT-116 compared to HT-29, but not on the folic acid-negative cells (FR−) as HCT-15. PPF-E NPs enhanced intracellular reactive oxygen species (ROS) level in absence of N-acetyl-l-cysteine (NAC), elevated DNA fragmentation level, and increased apoptotic cell death at higher doses compared to other two NPs and free EGCG. In conclusion, PPF-E NPs exerted greater efficacy than PP-E, P-E, and free EGCG in HCT-116 cells. [ABSTRACT FROM AUTHOR]

Cardiovascular diseases (CVDs), the world's most prominent cause of mortality, continue to be challenging conditions for patients, physicians, and researchers alike. CVDs comprise a wide range of illnesses affecting the heart, blood vessels, and the blood that flows through and between them. Advances in nanomedicine, a discipline focused on improving patient outcomes through revolutionary treatments, imaging agents, and ex vivo diagnostics, have created enthusiasm for overcoming limitations in CVDs' therapeutic and diagnostic landscapes. Nanomedicine can be involved in clinical purposes for CVD through the augmentation of cardiac or heart-related biomaterials, which can be functionally, mechanically, immunologically, and electrically improved by incorporating nanomaterials; vasculature applications, which involve systemically injected nanotherapeutics and imaging nanodiagnostics, nano-enabled biomaterials, or tissue-nanoengineered solutions; and enhancement of sensitivity and/or specificity of ex vivo diagnostic devices for patient samples. Therefore, this review discusses the latest studies based on applying organic nanoparticles in cardiovascular illness, including drug-conjugated polymers, lipid nanoparticles, and micelles. Following the revised information, it can be concluded that organic nanoparticles may be the most appropriate type of treatment for cardiovascular diseases due to their biocompatibility and capacity to integrate various drugs. [ABSTRACT FROM AUTHOR]

Polymeric particles less than 100 nm in size (polymer nanoparticles), which are useful in the fields of medicine and so on, are synthesized through emulsion polymerization, wherein surfactants are essential for maintaining their dispersion stability, contaminating particle surfaces and causing high environmental pollution. The soap‐free emulsion polymerization (SFEP) of styrene in a packed reactor using microglass beads enables the synthesis of polymer nanoparticles without surfactants. Ultraviolet irradiation is used for radical polymerization using an initiator during the SFEP of styrene. The reaction space in the packed reactor is controlled by the size of glass beads to be filled in the reactor. A decrease in the size of the glass beads narrows the reaction space, causing the average polystyrene particle size to reach 27.3 nm and suppress convection flow by the wall of the glass beads, thereby limiting particle motion and preventing particle growth through particle collisions. [ABSTRACT FROM AUTHOR]

Silybin (SIB) is a hepatoprotective drug known for its poor oral bioavailability, attributed to its classification as a class IV drug with significant metabolism during the first-pass effect. This study explored the potential of solid lipid nanoparticles with (SLN-SIB-U) or without (SLN-SIB) ursodeoxycholic acid and polymeric nanoparticles (PN-SIB) as delivery systems for SIB. The efficacy of these nanosystems was assessed through in vitro studies using the GRX and Caco-2 cell lines for permeability and proliferation assays, respectively, as well as in vivo experiments employing a murine model of Schistosomiasis mansoni infection in BALB/c mice. The mean diameter and encapsulation efficiency of the nanosystems were as follows: SLN-SIB (252.8 ± 4.4 nm, 90.28 ± 2.2%), SLN-SIB-U (252.9 ± 14.4 nm, 77.05 ± 2.8%), and PN-SIB (241.8 ± 4.1 nm, 98.0 ± 0.2%). In the proliferation assay with the GRX cell line, SLN-SIB and SLN-SIB-U exhibited inhibitory effects of 43.09 ± 5.74% and 38.78 ± 3.78%, respectively, compared to PN-SIB, which showed no inhibitory effect. Moreover, SLN-SIB-U demonstrated a greater apparent permeability coefficient (25.82 ± 2.2) than PN-SIB (20.76 ± 0.1), which was twice as high as that of SLN-SIB (11.32 ± 4.6) and pure SIB (11.28 ± 0.2). These findings suggest that solid lipid nanosystems hold promise for further in vivo investigations. In the murine model of acute-phase Schistosomiasis mansoni infection, both SLN-SIB and SLN-SIB-U displayed hepatoprotective effects, as evidenced by lower alanine amino transferase values (22.89 ± 1.6 and 23.93 ± 2.4 U/L, respectively) than those in control groups I (29.55 ± 0.7 U/L) and I+SIB (34.29 ± 0.3 U/L). Among the prepared nanosystems, SLN-SIB-U emerges as a promising candidate for enhancing the pharmacokinetic properties of SIB. [ABSTRACT FROM AUTHOR]

Over the past couple of decades, the incidence of breast cancer (BC) has significantly increased among females in comparison to other cancer types. In medicinal terminology, the susceptibility to BC is mainly centered around three hormonal receptors: estrogen (ER), progesterone (PR), and human epidermal growth receptor (HER2). Notably, estrogen- dependent breast cancer has a considerable female demographic, making it treatable with hormonal drugs and less intensive immunotherapy. Conversely, the narrative delves into the ominous type of cancer known as triple-negative breast cancer (TNBC). The orientation of all three receptors falls in a negative direction, which is ineffective for treatments that rely on hormonal or antagonist medicaments. Therefore, the only option available to tackle this type of cancer is chemotherapy, which causes toxicity within the body, is highly expensive, and is non-targeted. To counter this challenge, researchers have pioneered nano-based drug delivery systems (NDDS) owing to their innumerable merits and scientific development. NDDS mainly involves polymeric nanoparticles, liposomes, and dendrimers. This review comprehensively details the advancements in nanoinduced targeted drug delivery systems, with a focus on surface modification techniques for active targeting, enhanced drug release, and improved pharmacokinetics. Critical analysis extends to preclinical and clinical studies, revealing the potential of nano-drug delivery systems in TNBC to surpass traditional therapies, with promising heightened efficacy and reduced side effects. [ABSTRACT FROM AUTHOR]

Studies in which polymeric nanoparticles are used in drug delivery have been one of the subjects of interest in recent years. In this study, histidine-containing polymeric nanoparticles [poly(2-hydroxyethyl methacrylate-co-N-methacryloylamido histidine methyl ester)] were synthesized by surfactant free emulsion polymerization method. Ciprofloxacin was loaded onto the HPCNs surface [CIP-HCPNs]. In the characterization of CIP-HCPNs, scanning electron microscopy, Fourier-infrared analysis, surface area calculations and zeta potential analysis were used. FT-IR data of histidine-free polymeric nanoparticles [HFPNs] and HCPNs demonstrated the successful addition of Histidine to polymeric nanoparticles. SEM images showed that CIP-HCPNs had a size of 131.2 nm with a spherical shape. As a result of Zeta potential studies, the polydispersity index (PDI) of CIP-HCPNs was found to be 0.11, indicating that CIP-HCPNs have a narrowly spaced size distribution. CIP release from CIP-HCNPs showed slow-release properties. At pH 7.4, cumulative CIP release from CIP-HCPNs was 96% (283.35 mg/g) within 6 h, with full drug release achieved at 24 h. It was stated that the drug release kinetic data obtained from CIP release experiments fit the Hixson-Crowell model, and in this model, CIP release from CIP-HCPNs occurred as the square root of the time dependent process based on Fickian diffusion. As a result, CIP-HCNPs developed in the current study, it can be said that it is suitable for drug release. [ABSTRACT FROM AUTHOR]